PARP INHIBITOR VIII PJ34 1PC X 1MG (C005B-034237)

General description

A cell-permeable, water-soluble phenanthridinone-derivative that acts as a potent inhibitor of poly(ADP-ribose) polymerase (PARP; EC₅₀ = 20 nM). Shown to be about 10,000 times more potent than the prototypical PARP inhibitor, 3-Aminobenzamide (Cat. No. 165350; EC₅₀ = 200 µM). Does not act as an antioxidant at higher concentrations (1 µM to 10 mM). Exhibits neuroprotection in in vivo and in vitro models of stroke. Also available as a 20 mM solution in H₂O(Cat. No. 528151).

A water-soluble phenanthridinone-derivative that acts as a potent anti-inflammatory agent and an inhibitor of poly(ADP-ribose) polymerase (PARP; EC₅₀ = 20 nM). Shown to be about 10,000-fold more potent than the prototypical PARP inhibitor, 3-Aminobenzamide (Cat. No. 165350) (EC₅₀ = 200 µM). Suppresses neutrophil infiltration and nitric oxide production in peritonitis. Does not act as an antioxidant even at higher concentrations (1 µM to 10 µM). PJ34 inhibits peroxynitrite-induced cell necrosis with an (EC₅₀ = 20 nM). Exhibits neuroprotective effects in in vivo and in vitro models of stroke.

Biochem/physiol Actions

Cell permeable: yes

EC50 = 20 nM inhibiting poly(ADP-ribose) polymerase (PARP)

Primary Target
PARP

Product does not compete with ATP.

Reversible: no

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Abdelkarim, G.E., et al. 2001. Int. J. Mol. Med.7, 255.
Garcia-Soriano, F.G., et al. 2001. Nature Med. 7, 108.
Mabley, G.J., et al. 2001. Inflamm. Res.50, 561.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Molecular Weight: 295.34 (free base basis). Empirical Formula: C₁₇H₁₇N₃O₂ · xHCl. Quality Level: 100. Assay: ≥. 98% (HPLC). form: solid. manufacturer/tradename: Calbiochem^®. . storage condition: OK to freeze, desiccated (hygroscopic), protect from light. color: white. solubility: water: 5 . mg/mL. shipped in: ambient. storage temp.: −. 20°C. InChI: 1S/C17H17N3O2.ClH/c1-20(2)10-16(21)18-11-7-8-15-14(9-11)12-5-3-4-6-13(12)17(22)19-15. /h3-9H,10H2,1-2H3,(H,18,21)(H,19,22). 1H. InChI key: RURAZZMDMNRXMI-UHFFFAOYSA-N. Storage Class Code: 11 - Combustible Solids. WGK: WGK 3. Flash Point(F): Not applicable. Flash Point(C): Not applicable.